Search Results - "LIRAS, Jennifer L"
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Use of Immortalized Human Hepatocytes to Predict the Magnitude of Clinical Drug-Drug Interactions Caused by CYP3A4 Induction
Published in Drug metabolism and disposition (01-10-2006)“…Cytochrome P4503A4 (CYP3A4) is the principal drug-metabolizing enzyme in human liver. Drug-drug interactions (DDIs) caused by induction of CYP3A4 can result in…”
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2
In Vitro-In Vivo Extrapolation of Key Transporter Activity at the Blood-Brain Barrier
Published in Drug metabolism and disposition (01-04-2019)“…Understanding the quantitative implications of P-glycoprotein and breast cancer resistance protein efflux is a key hurdle in the design of effective, centrally…”
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3
Discovery of Potent and Selective Periphery-Restricted Quinazoline Inhibitors of the Cyclic Nucleotide Phosphodiesterase PDE1
Published in Journal of medicinal chemistry (24-05-2018)“…We disclose the discovery and X-ray cocrystal data of potent, selective quinazoline inhibitors of PDE1. Inhibitor (S)-3 readily attains free plasma…”
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Perspectives on the evaluation and adoption of complex in vitro models in drug development: Workshop with the FDA and the pharmaceutical industry (IQ MPS Affiliate)
Published in ALTEX, alternatives to animal experimentation (2022)“…Complex in vitro models (CIVM) offer the potential to improve pharmaceutical clinical drug attrition due to safety and/ or efficacy concerns. For this…”
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Strategies to minimize CNS toxicity: in vitro high-throughput assays and computational modeling
Published in Expert opinion on drug metabolism & toxicology (01-05-2012)“…Healthy functioning of the brain is dependent on the ability of the blood-brain barrier (BBB) and other central nervous system (CNS) barriers to protect the…”
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Harnessing Preclinical Data as a Predictive Tool for Human Brain Tissue Targeting
Published in ACS chemical neuroscience (17-03-2021)“…One of the objectives within the medicinal chemistry discipline is to design tissue targeting molecules. The objective of tissue specificity can be either to…”
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Considerations from an International Regulatory and Pharmaceutical Industry (IQ MPS Affiliate) Workshop on the Standardization of Complex In Vitro Models in Drug Development
Published in Advanced biology (01-08-2024)“…In May 2022, there is an International Regulatory and Pharmaceutical Industry (Innovation and Quality [IQ] Microphysiological Systems [MPS] Affiliate) Workshop…”
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8
Solid and Solution Phase Organic Syntheses of Oligomeric Thioureas
Published in Journal of organic chemistry (13-12-1996)“…In order to study supramolecular architectures built from unnatural oligomeric and polymeric structures, one must first have an efficient synthetic strategy to…”
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The Ratio between Endocyclic and Exocyclic Cleavage of Pyranoside Acetals Is Dependent upon the Anomer, the Temperature, the Aglycon Group, and the Solvent
Published in Journal of the American Chemical Society (03-09-1997)“…Several cis-fused decalin pyranosides with intramolecular nucleophiles of high effective molarity were studied to determine the ratio between endocyclic and…”
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10
Exocyclic and Endocyclic Cleavage of Pyranosides in Both Methanol and Water Detected by a Novel Probe
Published in Journal of the American Chemical Society (01-03-1994)Get full text
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11
Potent, selective pyrimidinetrione-based inhibitors of MMP-13
Published in Bioorganic & medicinal chemistry letters (15-11-2006)“…Using SAR from two related series of pyrimidinetrione-based inhibitors, compounds with potent MMP-13 inhibition and >100-fold selectivity against other MMPs…”
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Potent pyrimidinetrione-based inhibitors of MMP-13 with enhanced selectivity over MMP-14
Published in Bioorganic & medicinal chemistry letters (01-04-2005)“…[Display omitted] Through the use of computational modeling, a series of pyrimidinetrione-based inhibitors of MMP-13 was designed based on a lead inhibitor…”
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Potent, selective spiropyrrolidine pyrimidinetrione inhibitors of MMP-13
Published in Bioorganic & medicinal chemistry (01-12-2007)“…The discovery of novel, selective spirocyclic inhibitors of MMP-13 is reported. Explorations in the pyrimidinetrione series of MMP-13 inhibitors led to the…”
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14
Discovery of 3,3-dimethyl-5-hydroxypipecolic hydroxamate-based inhibitors of aggrecanase and MMP-13
Published in Bioorganic & medicinal chemistry letters (02-06-2005)“…A series of pipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was discovered based on screening known inhibitors of TNF-α converting enzyme (TACE)…”
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Discovery of 3-OH-3-methylpipecolic hydroxamates: Potent orally active inhibitors of aggrecanase and MMP-13
Published in Bioorganic & medicinal chemistry letters (15-07-2005)“…[Display omitted] A series of 3-hydroxy-3-methylpipecolic hydroxamate inhibitors of MMP-13 and aggrecanase was designed based on the observation of increased…”
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3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase
Published in Bioorganic & medicinal chemistry letters (20-09-2004)“…N-Hydroxy-3-hydroxy-4-arylsulfonyltetrahydropyranyl-3-carboxamides were designed as novel inhibitors of MMP-13 and aggrecanase based on known endocyclic…”
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17
Perspectives on the evaluation and adoption of complex in vitro models in drug development: Workshop with the FDA and the pharmaceutical industry (IQ MPS Affiliate)
Published in ALTEX (2022)“…Complex in vitro models (CIVM) offer the potential to improve pharmaceutical clinical drug attrition due to safety and/ or efficacy concerns. For this…”
Get more information
Journal Article